公开(公告)号：US07348339B2

公开(公告)日：2008-03-25

申请号：US10508760

申请日：2003-03-21

申请人： Nicholas Bailey ,  Mark James Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista B Goodman ,  Mark A Hilfiker ,  Dennis Lee ,  Terence Aaron Panchal ,  Robert A Stavenger ,  David Matthew Wilson ,  Jason Witherington

发明人： Nicholas Bailey ,  Mark James Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista B Goodman ,  Mark A Hilfiker ,  Dennis Lee ,  Terence Aaron Panchal ,  Robert A Stavenger ,  David Matthew Wilson ,  Jason Witherington

IPC分类号： A61K31/44 ,  A01N43/42 ,  C07D265/30 ,  C07D295/00 ,  C07D498/02

CPC分类号： C07D471/04

摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。 条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; X 7和X 8可以相同或不同，是选自N或CR 9的基团。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，并且选自N或C 11 ; 其制备方法，含有它们的药物组合物及其在医药中的用途。

公开(公告)号：US20050153978A1

公开(公告)日：2005-07-14

申请号：US10508592

申请日：2003-03-21

申请人： Michael Alberti ,  Stephen Garland ,  David Jung ,  James Veal ,  Jason Witherington

发明人： Michael Alberti ,  Stephen Garland ,  David Jung ,  James Veal ,  Jason Witherington

IPC分类号： A61K31/4184 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P43/00 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/06 ,  A61K31/4439 ,  A61K31/4709 ,  C07D43/14

CPC分类号： C07D403/04 ,  A61K31/4184 ,  C07D413/04 ,  C07D413/14 ,  C07D471/06

摘要： A method of treating an Msk-1 and/or ROCK(1 and 2) mediated disease or condition in a mammal comprising administration of an effective amount of a compounds of the formula (I) and physiologically acceptable salts thereof wherein, R1 is a 5, or 6 membered heterocyclic group selected from group a, b, c or d wherein X1 is a group selected from N or CR7 and X2 is a group selected from O, S or NR8; X3 and X4 which may be the same or different is a group selected from N or CR7; X5 is a group selected from O, S or NR8 and X6 is N or CR7; X7, X8 and X9 may be the same or different and selected from a group N or CR7, pharmaceutical compositions, novel compounds and processes for their preparation.

摘要翻译： 一种在哺乳动物中治疗Msk-1和/或ROCK（1和2）介导的疾病或病症的方法，包括施用有效量的式（I）化合物及其生理学上可接受的盐，其中R 1， 1是选自组a，b，c或d的5或6元杂环基团，其中X 1是选自N或CR 7的基团。 并且X 2是选自O，S或NR 8的基团。 X 3和X 4可以相同或不同，是选自N或CR 7的基团。 X 5是选自O，S或NR 8和X 6的基团是N或CR 7; X 7，X 8和X 9可以相同或不同，并且选自N或C 7 ，药物组合物，新化合物及其制备方法。

公开(公告)号：US07297792B2

公开(公告)日：2007-11-20

申请号：US11422338

申请日：2006-06-06

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

IPC分类号： C07D413/00

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US06776635B2

公开(公告)日：2004-08-17

申请号：US09881463

申请日：2001-06-14

申请人： Michael Allen Blanchfield ,  Michael Stephen Garland ,  Troy Everette Conner ,  James Charles Shiffler

发明人： Michael Allen Blanchfield ,  Michael Stephen Garland ,  Troy Everette Conner ,  James Charles Shiffler

IPC分类号： H01R1353

CPC分类号： H01R12/7088 ,  H01R12/58 ,  H01R12/724

摘要： A multi-beam power contact is provided including a main body and a plurality of at least three beams, which may be grouped in beam pairs, extending from the main body. The beams are adapted for mating with a mating connector, and the beams comprise contact areas adapted for electrical connection with the mating connector. Additionally, the multi-beam power contact may optionally include at least one initial contact beam and at least one non-initial contact beam. The initial contact beam is arranged to electrically connect to the mating connector before the non-initial contact beam electrically connects while the multi-beam power contact is being mated.

摘要翻译： 提供了一种多光束电力接触器，其包括主体和多个至少三个光束，所述至少三个光束可以从所述主体延伸出来，所述至少三个光束可以被分组成光束对。 梁适于与配合连接器配合，并且梁包括适于与配合连接器电连接的接触区域。 另外，多光束功率接触可以可选地包括至少一个初始接触光束和至少一个非初始接触光束。 初始接触梁布置成在多束电力接触件配合之前非初始接触梁电连接之前电连接到配合连接器。

公开(公告)号：US20060223800A1

公开(公告)日：2006-10-05

申请号：US11422338

申请日：2006-06-06

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US07109199B2

公开(公告)日：2006-09-19

申请号：US10381292

申请日：2001-09-19

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Bernadette Hickey ,  John Liddle ,  David Glynn Smith ,  Robert William Ward ,  Jason Witherington

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/4162 ,  A61P3/10

CPC分类号： C07D471/04 ,  C07D213/85 ,  C07D487/04

摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.

摘要翻译： 本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可各自独立地为未取代或取代的未取代或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自独立地为未取代或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明包括制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

公开(公告)号：US20050197328A1

公开(公告)日：2005-09-08

申请号：US10508760

申请日：2003-03-21

申请人： Nicholas Bailey ,  Mark Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista Goodman ,  Mark Hilfiker ,  Dennis Lee ,  Terence Panchal ,  Robert Stavenger ,  David Wilson ,  Jason Witherington

发明人： Nicholas Bailey ,  Mark Bamford ,  Haifeng Cui ,  Stephen Garland ,  Krista Goodman ,  Mark Hilfiker ,  Dennis Lee ,  Terence Panchal ,  Robert Stavenger ,  David Wilson ,  Jason Witherington

IPC分类号： C07D473/36 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5377 ,  A61P1/04 ,  A61P11/06 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D471/04 ,  A61K31/551 ,  A61K31/498 ,  A61K31/503 ,  C07D473/14 ,  C07D487/02

CPC分类号： C07D471/04

摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。 条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; 可以相同或不同的是选自N或CR 9的基团;其中X 1和X 3可以相同或不同。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，选自基团N或CR 13， 11 其制备方法，含有它们的药物组合物及其在医药中的用途。

公开(公告)号：US06805591B2

公开(公告)日：2004-10-19

申请号：US10041298

申请日：2002-01-08

申请人： Michael Stephen Garland ,  Daniel Robert Ringler ,  James Charles Shiffler

发明人： Michael Stephen Garland ,  Daniel Robert Ringler ,  James Charles Shiffler

IPC分类号： H01R1340

CPC分类号： H01R12/7088

摘要： A connector housing having a contact secured therein is provided. The connector housing includes inner walls that define a contact-receiving chamber. The contact-receiving chamber includes a channel along at least a portion of one of the inner walls for receiving a contact retention member. The contact-receiving chamber may include multiple channels for receiving multiple contact retention members. The contact includes a body section having the contact retention member thereon. The contact may include multiple body sections. The contact retention member includes a bulge portion flared outward in a direction transverse to the body section. The contact retention member may include multiple bulge portions and the multiple bulge portions may flare outward and inward in opposite directions from one another. When the contact is loaded into the housing and the contact retention member is received by the channel, the bulge portion frictionally engages at least one of the inner walls of the contact-receiving chamber. The frictional engagement of the bulge portion to at least one of the inner walls secures the contact within the connector housing.

摘要翻译： 提供具有固定在其中的接触件的连接器壳体。 连接器壳体包括限定接触容纳室的内壁。 接触接收室包括沿内壁之一的至少一部分的通道，用于接收接触保持构件。 接触接收室可以包括用于接收多个接触保持构件的多个通道。 接触件包括其上具有接触保持构件的主体部分。 触点可以包括多个主体部分。 接触保持构件包括在横向于主体部分的方向上向外张开的凸起部分。 接触保持构件可以包括多个凸起部分，并且多个凸起部分可以彼此相反的方向向外和向内张开。 当接触件被装载到壳体中并且接触保持构件被通道接收时，凸起部分摩擦地接合接触接收室的内壁中的至少一个。 凸起部分与至少一个内壁的摩擦接合将接触件固定在连接器壳体内。